MA38012A1 - Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 - Google Patents
Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5Info
- Publication number
- MA38012A1 MA38012A1 MA38012A MA38012A MA38012A1 MA 38012 A1 MA38012 A1 MA 38012A1 MA 38012 A MA38012 A MA 38012A MA 38012 A MA38012 A MA 38012A MA 38012 A1 MA38012 A1 MA 38012A1
- Authority
- MA
- Morocco
- Prior art keywords
- modulators
- ethynyl derivatives
- receptor activity
- mglur5 receptor
- disease
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Epidemiology (AREA)
Abstract
La présente invention concerne des dérivés d'éthynyle de formule (i) dans laquelle y est un groupe n ou ch, r1 est un groupe fluoro ou chloro, r2 est un groupe hydrogène ou méthyle ou leur sel d'addition aux acides pharmaceutiquement acceptable, leur mélange racémique, ou leur énantiomère et/ou isomère optique et/ou stéréoisomère correspondant. Il a été découvert avec surprise que les composés de formule générale i sont des antagonistes des récepteurs métabotropes au glutamate (modulateurs allostériques négatifs) destinés à être utilisés dans le traitement de l'anxiété et de la douleur, de la dépression, du syndrome de l'x fragile, des troubles du spectre autistique, de la maladie de parkinson et de la maladie du reflux gastro-oesophagien).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12188940 | 2012-10-18 | ||
| PCT/EP2013/071500 WO2014060398A1 (fr) | 2012-10-18 | 2013-10-15 | Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA38012A1 true MA38012A1 (fr) | 2016-05-31 |
| MA38012B1 MA38012B1 (fr) | 2016-12-30 |
Family
ID=47049067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA38012A MA38012B1 (fr) | 2012-10-18 | 2015-04-17 | Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US9227959B2 (fr) |
| EP (1) | EP2909180B1 (fr) |
| JP (1) | JP5989250B2 (fr) |
| KR (1) | KR101684816B1 (fr) |
| CN (1) | CN104718192B (fr) |
| AR (1) | AR093042A1 (fr) |
| AU (1) | AU2013333988B2 (fr) |
| BR (1) | BR112015006454A8 (fr) |
| CA (1) | CA2882520A1 (fr) |
| CL (1) | CL2015000891A1 (fr) |
| CO (1) | CO7200248A2 (fr) |
| CR (1) | CR20150144A (fr) |
| EA (1) | EA025667B1 (fr) |
| ES (1) | ES2599553T3 (fr) |
| IL (1) | IL237380A (fr) |
| MA (1) | MA38012B1 (fr) |
| MX (1) | MX2015004898A (fr) |
| MY (1) | MY168937A (fr) |
| NZ (1) | NZ705144A (fr) |
| PE (1) | PE20150629A1 (fr) |
| PH (1) | PH12015500398B1 (fr) |
| SG (1) | SG11201501392TA (fr) |
| TW (1) | TWI490208B (fr) |
| UA (1) | UA114529C2 (fr) |
| WO (1) | WO2014060398A1 (fr) |
| ZA (1) | ZA201500856B (fr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104603110B (zh) * | 2012-10-18 | 2016-08-31 | 霍夫曼-拉罗奇有限公司 | 作为mGluR5受体活性的调节剂的乙炔基衍生物 |
| JP6603334B2 (ja) * | 2015-06-03 | 2019-11-06 | エフ．ホフマン−ラ ロシュ アーゲー | エチニル誘導体 |
| WO2017053769A1 (fr) * | 2015-09-25 | 2017-03-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Utilisation de dérivés de triazole comme antagonistes du récepteur p2y14 |
| ES2897050T3 (es) | 2017-12-08 | 2022-02-28 | Boehringer Ingelheim Int | Derivados de imidazopiridina y el uso de los mismos como medicamento |
| JP7093469B2 (ja) | 2018-10-17 | 2022-06-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４－ピリジニルメチル－モルホリン誘導体および医薬としてのその使用 |
| TW202035395A (zh) * | 2018-10-17 | 2020-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 4-嘧啶-5-基甲基-嗎啉衍生物及其作為藥物之用途 |
| PE20211278A1 (es) * | 2018-10-17 | 2021-07-19 | Boehringer Ingelheim Int | Derivados de 4-pirazin-2-ilmetil-morfolina y su uso como medicamento |
| US12398143B2 (en) | 2019-06-04 | 2025-08-26 | Boehringer Ingelheim International Gmbh | Imidazopyrazine derivatives and the use thereof as medicament |
| WO2020245136A1 (fr) | 2019-06-04 | 2020-12-10 | Boehringer Ingelheim International Gmbh | Dérivés de purine, utilisés en tant que modulateurs négatifs de nr2b et leur utilisation en tant que médicament, en particulier pour le traitement de troubles dépressifs |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| UA80888C2 (en) * | 2003-06-05 | 2007-11-12 | Hoffmann La Roche | Imidazole derivatives as glutmate receptor antagonists |
| EP2162136A4 (fr) * | 2007-06-03 | 2012-02-15 | Univ Vanderbilt | Dérivés benzamides modulateurs allostériques positifs récepteurs métabotropiques du glutamate 5 (mglur5) et leurs procédés de fabrication et d'utilisation |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| WO2013049255A1 (fr) * | 2011-09-26 | 2013-04-04 | Vanderbilt University | Analogues de 5-(prop-1-yn-1-yl)picolinamide substitué comme modulateurs allostériques des récepteurs de mglur5 |
-
2013
- 2013-10-15 SG SG11201501392TA patent/SG11201501392TA/en unknown
- 2013-10-15 UA UAA201504680A patent/UA114529C2/uk unknown
- 2013-10-15 CN CN201380053660.XA patent/CN104718192B/zh not_active Expired - Fee Related
- 2013-10-15 MX MX2015004898A patent/MX2015004898A/es unknown
- 2013-10-15 BR BR112015006454A patent/BR112015006454A8/pt not_active Application Discontinuation
- 2013-10-15 JP JP2015535066A patent/JP5989250B2/ja not_active Expired - Fee Related
- 2013-10-15 EA EA201590699A patent/EA025667B1/ru not_active IP Right Cessation
- 2013-10-15 WO PCT/EP2013/071500 patent/WO2014060398A1/fr not_active Ceased
- 2013-10-15 MY MYPI2015000470A patent/MY168937A/en unknown
- 2013-10-15 PE PE2015000396A patent/PE20150629A1/es active IP Right Grant
- 2013-10-15 NZ NZ705144A patent/NZ705144A/en not_active IP Right Cessation
- 2013-10-15 KR KR1020157009544A patent/KR101684816B1/ko not_active Expired - Fee Related
- 2013-10-15 CA CA2882520A patent/CA2882520A1/fr not_active Abandoned
- 2013-10-15 ES ES13783003.0T patent/ES2599553T3/es active Active
- 2013-10-15 EP EP13783003.0A patent/EP2909180B1/fr active Active
- 2013-10-15 AU AU2013333988A patent/AU2013333988B2/en not_active Ceased
- 2013-10-17 TW TW102137560A patent/TWI490208B/zh not_active IP Right Cessation
- 2013-10-17 AR ARP130103764A patent/AR093042A1/es unknown
-
2015
- 2015-02-05 ZA ZA2015/00856A patent/ZA201500856B/en unknown
- 2015-02-16 CO CO15032736A patent/CO7200248A2/es unknown
- 2015-02-23 IL IL237380A patent/IL237380A/en not_active IP Right Cessation
- 2015-02-24 PH PH12015500398A patent/PH12015500398B1/en unknown
- 2015-03-18 CR CR20150144A patent/CR20150144A/es unknown
- 2015-04-09 CL CL2015000891A patent/CL2015000891A1/es unknown
- 2015-04-17 MA MA38012A patent/MA38012B1/fr unknown
- 2015-04-17 US US14/689,375 patent/US9227959B2/en active Active
Also Published As
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